US7208600B2 - Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases - Google Patents

Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases Download PDF

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Publication number
US7208600B2
US7208600B2 US10/964,214 US96421404A US7208600B2 US 7208600 B2 US7208600 B2 US 7208600B2 US 96421404 A US96421404 A US 96421404A US 7208600 B2 US7208600 B2 US 7208600B2
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United States
Prior art keywords
formula
compounds
aliphatic
ring
hcv
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Expired - Fee Related, expires
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US10/964,214
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English (en)
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US20050137140A1 (en
Inventor
Kevin M. Cottrell
Robert B. Perni
Janos Pitlik
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Priority to US10/964,214 priority Critical patent/US7208600B2/en
Publication of US20050137140A1 publication Critical patent/US20050137140A1/en
Assigned to VERTEX PHARMACEUTICALS INCORPORATED reassignment VERTEX PHARMACEUTICALS INCORPORATED ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: PITLIK, JANOS, COTTRELL, KEVIN, PERNI, ROBERT
Priority to US11/716,248 priority patent/US8039623B2/en
Application granted granted Critical
Publication of US7208600B2 publication Critical patent/US7208600B2/en
Assigned to MACQUARIE US TRADING LLC reassignment MACQUARIE US TRADING LLC SECURITY INTEREST Assignors: VERTEX PHARMACEUTICALS (SAN DIEGO) LLC, VERTEX PHARMACEUTICALS INCORPORATED
Assigned to VERTEX PHARMACEUTICALS INCORPORATED, VERTEX PHARMACEUTICALS (SAN DIEGO) LLC reassignment VERTEX PHARMACEUTICALS INCORPORATED RELEASE BY SECURED PARTY (SEE DOCUMENT FOR DETAILS). Assignors: MACQUARIE US TRADING LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
US10/964,214 2003-10-10 2004-10-12 Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases Expired - Fee Related US7208600B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US10/964,214 US7208600B2 (en) 2003-10-10 2004-10-12 Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases
US11/716,248 US8039623B2 (en) 2003-10-10 2007-03-09 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US51015603P 2003-10-10 2003-10-10
US51376803P 2003-10-23 2003-10-23
US10/964,214 US7208600B2 (en) 2003-10-10 2004-10-12 Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US11/716,248 Continuation US8039623B2 (en) 2003-10-10 2007-03-09 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

Publications (2)

Publication Number Publication Date
US20050137140A1 US20050137140A1 (en) 2005-06-23
US7208600B2 true US7208600B2 (en) 2007-04-24

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US10/964,214 Expired - Fee Related US7208600B2 (en) 2003-10-10 2004-10-12 Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases
US11/716,248 Expired - Fee Related US8039623B2 (en) 2003-10-10 2007-03-09 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

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US11/716,248 Expired - Fee Related US8039623B2 (en) 2003-10-10 2007-03-09 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

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US (2) US7208600B2 (US08039623-20111018-C00020.png)
EP (2) EP1692157B1 (US08039623-20111018-C00020.png)
JP (2) JP2007532474A (US08039623-20111018-C00020.png)
KR (2) KR20060130027A (US08039623-20111018-C00020.png)
CN (1) CN101857631A (US08039623-20111018-C00020.png)
AU (1) AU2004282148A1 (US08039623-20111018-C00020.png)
CA (1) CA2541634A1 (US08039623-20111018-C00020.png)
IL (1) IL174863A0 (US08039623-20111018-C00020.png)
MX (1) MXPA06004006A (US08039623-20111018-C00020.png)
NO (1) NO20062101L (US08039623-20111018-C00020.png)
NZ (1) NZ546663A (US08039623-20111018-C00020.png)
RU (1) RU2006115558A (US08039623-20111018-C00020.png)
TW (1) TW200528472A (US08039623-20111018-C00020.png)
WO (1) WO2005037860A2 (US08039623-20111018-C00020.png)

Cited By (74)

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US20050080017A1 (en) * 2003-10-10 2005-04-14 Cottrell Kevin M. Inhibitors of serine proteases, particularly HVC NS3-NS4A protease
US20050197299A1 (en) * 2000-08-31 2005-09-08 Babine Robert E. Peptidomimetic protease inhibitors
US20050215486A1 (en) * 2004-02-04 2005-09-29 Kevin Cottrell Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US20060003942A1 (en) * 2003-10-27 2006-01-05 Roger Tung Combinations for HCV treatment
US20060211629A1 (en) * 2003-07-18 2006-09-21 Britt Shawn D Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US20070054842A1 (en) * 2005-07-25 2007-03-08 Blatt Lawrence M Novel macrocyclic inhibitors of hepatitis C virus replication
US20070161789A1 (en) * 2003-10-10 2007-07-12 Cottrell Kevin M Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US20070179167A1 (en) * 2005-08-26 2007-08-02 Cottrell Kevin M Inhibitors of serine proteases
US20080019942A1 (en) * 2006-07-05 2008-01-24 Intermune, Inc Novel inhibitors of hepatitis c virus replication
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